Burger′s Medicinal Chemistry, Drug Discovery, and Development

Donald Abraham is an Emeritus Professor of Medicinal Chemistry and Emeritus Director of the Institute for Structural Biology and Drug Discovery at Virginia Commonwealth University. He was the sole Editor-in-Chief on the 6th edition of Burger's. In 2010, Dr. Abraham was elected to the Hall of Fame of the American Chemical Society's Medicinal Chemistry Division. David Rotella is a Principal Research Scientist at Wyeth Research. He is the Chair of the American Chemical Society Division of Medicinal Chemistry for 2007.

Volume 1: Methods in Drug Discovery. History of Quantitative Structure Activity Relationships. Mass spectrometry and drug discovery. Chirality and Biological Activity. Analog design. SNPs: Single Nucleotide Polymorphisms and Pharmacogenomics - individually designed drug therapy. Design of peptidomimetics. Dual Acting Drugs. Combinational chemistry and multiple parallel synthesis. Allosteric proteins and drug discovery. Principles of drug metabolism. Pharmacophore-based drug design. Use of biological fingerprints vs Structure/chemotypes to describe molecules. Recent advances in development, validation and exploitation of QSAR models. The Application of recombinant DNA Technology in medicinal chemistry and drug discovery. Structural genomics, its application in Chemistry, Biology, Medicine, and Drug Discovery. Volume 2: Discovering Lead Molecules. Virtual screening. Utility and applications of in vitro ADMET profiling in lead discovery. Retrometabolism-Based Drug Design and Targeting. Natural product screening. Microbes to man; from the depths to drugs. Multi-objective Optimization For Drug Discovery. GPCR homology model development and applications. Structural Alerts for Toxicity. Protein - Protein Interactions as Drug Discovery Targets. NMR-based Screening and Drug Discovery. Membrane transport proteins and drug transport. Receptor targets in drug discovery and development. Selective Toxicities. Chemogenomics - Systematization of Drug Discovery. Docking and Scoring in Drug Discovery. Recent Trends in Structure-Based Drug Design and Energetics. QM and QM/MM Approaches to Evaluating Binding Affinities. Assessing the Bioavailability of Drug Delivery Systems: Mathematical Modeling. Protein flexibility in in silico screening. Volume 3: Drug Development. Large scale and scale up synthesis. Physicochemical characterization and principles of oral dosage form selection. The FDA and drug regulatory issues. Intellectual property in drug discovery and biotechnology. Polymorphism and conjugation in drug delivery (crystal engineering). Prodrugs: Strategic Deployment, Metabolic Considerations and Chemical Design Principles. Process Development of Protein Therapeutics. Cost-Effectiveness Analyses throughout the Drug Development Life Cycle. Provisional BCS Classification of the Leading Oral Drugs on the Global Market. The role of permeability in drug ADME/PK, interactions and toxicity, and the Permeability-based Classification System (PCS). Salt screening and selection. Enzymatic assays for HTS or Assay Development for HTS. Crystallographic Survey of the Endogenous Albumin Drug Transport System and its Application in Cancer Chemotherapy. Nanotechnology in pharmaceuticals. Volume 4: Cardiovascular, Endocrine and Metabolic Diseases. Diabetes Drugs and Emerging Targets. DPP-4 inhibitors. Nuclear hormone receptor medicinal chemistry. Thyroid hormones and thyromimetics. Antihypertensives:renin inhibitors. Antihypertensives - Angiotensin-converting enzyme inhibitors. Atherosclerosis I: LDL Cholesterol Lowering. Atherosclerosis I: HDL Elevation. Anticoagulants. Antiplatelets. Congestive Heart Failure. Endogenous vasoactive peptides. Hematopoietic agents. Oxygen delivery via allosteric effectors of hemoglobin and blood substitutes. Volume 5: Pulmonary, Bone, Immunology, Vitamins and Autocoid Therapeutic Agents. Fundamentals of steroid chemistry and biochemistry. Antiinflammatory Glucocorticoids. Male sex hormones, analogs, and antagonists. Female Sex Hormones (pick up from the online). Medicinal chemistry and therapeutic applications of the gaseotransmitters NO, CO and H2S and their prodrugs. Retinoids. Multiple sclerosis. Ophthalmic agents. Vitamins. Drug Discovery in Non-Life Threatening Disorders: Erectile Dysfunction, Insomnia and Smoking Cessation. Osteoporosis therapy: mechanistic antiresoptives. Osteoporosis therapy: anabolics. Current and Emerging Therapies in Chronic Obstructive Pulmonary Disease. Agents acting on prostanoid & TX receptors. Therapeutic agents acting on RNA. Immunosuppressive agents for the prevention of transplantation rejection. Volume 6: Cancer. Natural product cytotoxics. Histone Deacetylase Inhibitors: A brief overview of their role and medicinal chemistry. Synthetic DNA-targeted chemotherapeutic agents and related tumor-activated prodrugs. PARP Inhibitors as Anticancer Agents. Proteasome inhibitors. CNS Cancers. Kinase inhibitors: Approved Drugs and Clinical Candidates. Structure-Based Design of Kinase Inhibitors: Molecular Recognition of Protein Multiple Conformations. Cancer drug resistance-targets and therapies. HSP inhibitors. Gene therapy with plasmid DNA. Volume 7: Antiinfectives. The FDA Approved HIV-1 Protease Inhibitors for Treatment of HIV/AIDS. HIV integrase. CCR5 Antagonists. Reverse Transcriptase Inhibitors (RTIs). Anti HCV agents. Anti-DNA Virus Agents. B-lactam antibiotics-include monobactams, b-lactamase inhibitors. Tetracyclines, aminoglycoside, macrolide, and miscellaneous antibiotics. Synthetic antibacterial agents. Antiprotozoal/ Antiparasitic Agents. Antimalarials. Anti-tuberculosis. Volume 8: CNS Disorders. Chemical Perspective on Neurotransmission and Drug Discovery for the Central Nervous System. Cognition. Cholinergics/anticholinergics/muscarinics/nicotinics. CNS stimulants. Anticonvulsants. Antipsychotic agents. Antidepressants. Therapeutic Agents for the Treatment of Migraine. Approaches to Amyloid Therapies for the Treatment of Alzheimers Disease. Non-Amyloid Approaches to Alzheimer's Disease. Stroke. Therapeutic and Diagnostic Agents for Parkinson?s Disease. Opioid Receptor Ligands. PET and SPECT in Drug Development.